Derek J Parks
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Explore the profile of Derek J Parks including associated specialties, affiliations and a list of published articles.
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24
Citations
1921
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Recent Articles
1.
Smalley Jr T, Boggs S, Caravella J, Chen L, Creech K, Deaton D, et al.
Bioorg Med Chem Lett
. 2014 Dec;
25(2):280-4.
PMID: 25499883
The farnesoid X receptor (FXR) may play a crucial role in a number of metabolic diseases and, as such, could potentially serve as a target for the development of therapeutics...
2.
Shotwell J, Baskaran S, Chong P, Creech K, Crosby R, Dickson H, et al.
ACS Med Chem Lett
. 2014 Jun;
3(7):565-9.
PMID: 24900511
A series of imidazo[1,2-a]pyridines which directly bind to HCV Non-Structural Protein 4B (NS4B) is described. This series demonstrates potent in vitro inhibition of HCV replication (EC50 < 10 nM), direct...
3.
Akwabi-Ameyaw A, Caravella J, Chen L, Creech K, Deaton D, Madauss K, et al.
Bioorg Med Chem Lett
. 2011 Sep;
21(20):6154-60.
PMID: 21890356
To further explore the optimum placement of the acid moiety in conformationally constrained analogs of GW 4064 1a, a series of stilbene replacements were prepared. The benzothiophene 1f and the...
4.
Bass J, Caravella J, Chen L, Creech K, Deaton D, Madauss K, et al.
Bioorg Med Chem Lett
. 2011 Jan;
21(4):1206-13.
PMID: 21256005
To improve on the drug properties of GSK8062 1b, a series of heteroaryl bicyclic naphthalene replacements were prepared. The quinoline 1c was an equipotent FXR agonist with improved drug developability...
5.
Grant D, Yin L, Collins J, Parks D, Orband-Miller L, Wisely G, et al.
ACS Chem Biol
. 2010 Aug;
5(10):925-32.
PMID: 20677822
The identification of nonporphyrin ligands for the orphan nuclear receptor Rev-erbα will enable studies of its role as a heme sensor and regulator of metabolic and circadian signaling. We describe...
6.
Phelan C, Gampe Jr R, Lambert M, Parks D, Montana V, Bynum J, et al.
Nat Struct Mol Biol
. 2010 Jun;
17(7):808-14.
PMID: 20581824
Repression of gene transcription by the nuclear receptor Rev-erbalpha plays an integral role in the core molecular circadian clock. We report the crystal structure of a nuclear receptor-co-repressor (N-CoR) interaction...
7.
Marino Jr J, Kallander L, Ma C, Oh H, Lee D, Gaitanopoulos D, et al.
Bioorg Med Chem Lett
. 2009 Sep;
19(19):5617-21.
PMID: 19717304
The liver X receptors (LXR) play a key role in cholesterol homeostasis and lipid metabolism. SAR studies around tertiary-amine lead molecule 2, an LXR full agonist, revealed that steric and...
8.
Akwabi-Ameyaw A, Bass J, Caldwell R, Caravella J, Chen L, Creech K, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4733-9.
PMID: 19586769
Two series of conformationally constrained analogs of the FXR agonist GW 4064 1 were prepared. Replacement of the metabolically labile stilbene with either benzothiophene or naphthalene rings led to the...
9.
Bass J, Caldwell R, Caravella J, Chen L, Creech K, Deaton D, et al.
Bioorg Med Chem Lett
. 2009 May;
19(11):2969-73.
PMID: 19410460
Starting from the known FXR agonist GW 4064 1a, a series of alternately 3,5-substituted isoxazoles was prepared. Several of these analogs were potent full FXR agonists. A subset of this...
10.
Washburn D, Hoang T, Campobasso N, Smallwood A, Parks D, Webb C, et al.
Bioorg Med Chem Lett
. 2009 Jan;
19(4):1097-100.
PMID: 19167885
A novel series of 1H-indol-1-yl tertiary amine LXR agonists has been designed. Compounds from this series were potent agonists with good rat pharmacokinetic parameters. In addition, the crystal structure of...